Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, and a are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically -acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: This invention relates to novel azabicyclo[3.2.1]oct-2-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: [Problems] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [Means for Solving Problems] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms —CH2-CH2- or the like, or M4 together with M2 or M3 forms —CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one —CH2- or —CH2-CH2- group is formed thereamong.

Abstract: This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: This invention relates to novel (1R,2R,3S,5S)-2-methoxymethyl-3-(3,4-dichlorophenyl)-8-azabicyclo[3.2.1]octane tartrate salts, such as L-tartrate monohydrates and anhydrates, wherein the salts are useful as monoamine neurotransmitter re-uptake inhibitors. Additionally, the invention also relates to the use of these salts in a method for therapy and to pharmaceutical compositions comprising the salts of the invention.

Abstract: Herein disclosed is a method of rescuing gonadotropin-releasing hormone receptor (GnRHR) mutants with IN3 or a mimetic thereof. IN3 significantly rescues 11 missense mutations as assessed by radioligand binding and by IP production. Such rescue occurred despite widely disparate loci along the receptor. In addition, many altered GnRH receptors (terminally truncated, internal deletions, or lacking the ability to form bridges to form tertiary structure) were rescued with IN3.

Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]oct-6-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: Compounds of formula I: selectively inhibit production of A?(1-42) and hence are useful in treatment or prevention of disease associated with deposition of ?-amyloid in the brain.

Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Abstract: Disclosed herein is a novel class of aminophenyl compounds having the structure: wherein R1 is cyano or nitro and ring A is a bi- or tricyclic bridged heterocycle and to their use as modulators of androgen receptor for the treatment or prevention of conditions relating thereto.

Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Disclosed herein is a novel class of aminophenyl compounds having the structure: wherein R1 is cyano or nitro and ring A is a bi- or tricyclic bridged heterocycle and to their use as modulators of androgen receptor for the treatment or prevention of conditions relating thereto.

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract: The present invention provides novel tropane compounds and methods for their use.

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Abstract: A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to a process for preparing a 2-(ethoxymethyl)-tropane derivative or a pharmaceutically acceptable salt thereof, by reacting the corresponding 2-(hydroxymethyl)-tropane derivative with ethyl bromide in the presence of a base, and a phase transfer catalyst.

Abstract: This invention relates to novel enantiomers useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: New antagonists of the interaction between the CCR1 Chemokine receptor and its ligands, including MIP-1? (CCL3), represented by formula (I) are disclosed, as well as pharmaceutical compositions comprising them and their use in therapy for the treatment of pathological conditions or diseases susceptible of being improved by antagonism of the CCR1 receptor.

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, and a are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]oct-6-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The present invention provides novel tropane compounds and methods for their use.

Abstract: The present invention provides a method for the N-demethylation of an N-methylated heterocycle, particularly a morphine or tropane alkaloid or derivative thereof. The method comprises reacting the heterocycle with a metal catalyst and a solvent in the presence of an oxidizing agent.

Abstract: The present invention relates to a process for preparing substituted 8-azabicyclo[3.2.1]octan-3-ols having the structural formula I or a pharmaceutically acceptable salt or solvate thereof, wherein R is benzyl, R5-benzyl, allyl, —C(O)R6, —C(O)OR8 or —CH(R7)2; R1 is optionally substituted aryl or optionally substituted heteroaryl; and R5, R6, R7 and R8 are as defined in the specification; comprising a) reacting an amine of formula II R—NH2??II with 2,5-dimethoxytetrahydrofuran or HC(O)(CH2)2C(O)H, and C(O)(CH2C(O)OR4)2, wherein R4 is H or alkyl, to obtain a compound of formula III b) reacting a compound of formula III with I-R1, alkyl lithium, and optionally a lithium salt, to obtain a compound of formula I; and c) optionally converting a compound of formula I wherein R is benzyl, R5-benzyl, allyl, —C(O)R6 or —C(O)OR8 to a compound of formula I wherein R is —CH(R7)2. Intermediates in the process are also claimed.

Abstract: Disclosed are benztropinamine analogs having the formula I (I) in which E is NR1, S, or CH2; B is NR4, O, or CH2; m=1 to 5; n=1 to 3; Ar is a C5-C20 monocyclic aryl group or a C10-C20 bicyclic aryl group or a heteroaryl group having 2 to 6 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, and any combination thereof; and bond “a” can be of ?, ?, or ?/? configuration, wherein R1 to R5 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.

Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract: Disclosed are tropane-based prodrug compounds bearing fatty ester and aromatic substituents. The compounds can be used for alleviating symptoms of CNS disorders.

Abstract: The present invention is directed to novel Muscarinic Acetylcholine receptor antagonists of Formula (I), pharmaceutical compositions and methods of using them. Compounds of Formula (I) are, inter alia, wherein: R1 and R2 are, independently, selected from the group consisting of 3-thienyl, pyridyl, benzyl, pyrimidyl, thiazolyl, isothiazolyl and C3-7cycloalkyl.

Abstract: Disclosed are benztropine analogs having the formula (I) in which Ar is a C6-C20 monocyclic aryl group or a C10-C20>bicyclic aryl group or a heteroaryl, heterocyclic, or arylheterocyclic group having 2 to 12 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, P, and any combination thereof; m=1 to 5; n=1 to 3; and R1 to R4 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.

Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The invention provides a process for preparation of a fluorohaloalkane, preferably an [18F]fluorohaloalkane of formula (I) wherein X is halo and n is an integer of from 1 to 6; which comprises: reaction of the corresponding organosilicon compound of formula (II): wherein n is as defined for the compound of formula (I); and R?, R?, and R?? are independently selected from C1-6 alkyl and C1-6 haloalkyl; and R? may alternatively be the group: with a compound of formula (III): wherein X is as defined for the compound of formula (I) and Y is halo. Intermediates having use in such processes are also claimed.

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: The present invention relates to the use of tropane derivatives having dopamine reuptake inhibitor activity for the treatment of diseases associated with reduced blood flow to the brain or with instances of a temporary break in blood supply to the brain, such as ischemic diseases.

Abstract: This invention relates to novel azacyclic ethynyl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention describes a method for the treatment of attention deficit hyperactivity disorder (ADHD), conduct disorder, alcohol addiction, tobacco addiction, nicotine addiction, parkinsonism including Parkinson's disease, female and male orgasmic disorders, female and male sexual arousal disorders, hypoactive sexual desire disorder, and disorders characterized by anxiety and/or depression. In this method, a therapeutically effective, nontoxic dose of a 4?,4?-substituted 3?-(diphenylmethoxy) tropane analog or a pharmaceutically acceptable salt thereof is administered to the patient in need of such treatment.